1445879-21-9|GSK 2837808A|CsnPharm

CAS No.: 1445879-21-9

GSK2837808A Catalog No. CSN28430

Synonyms: GSK-2837808

GSK2837808A is a potent and selective LDHA and LDHB inhibitor with IC50 values of 2.6nM and 43nM for LDHA and LDHB, respectively. It reduces glucose uptake and enhances mitochondrial oxygen consumption in Snu398 hepatocellular carcinoma cells.

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技术信息

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描述Lactate dehydrogenase (LDH) is an essential metabolic enzyme that catalyzes the interconversion of pyruvate and lactate using NADH/NAD(+) as a co-substrate^[2]. Lactate dehydrogenase A (LDHA) is a critical metabolic enzyme belonging to a family of 2-hydroxy acid oxidoreductases that plays a key role in anaerobic metabolism in the cells. In hypoxia condition, the overexpression of LDHA shifts the metabolic pathway of ATP synthesis from oxidative phosphorylation to aerobic glycolysis and the hypoxia condition is a common phenomenon occurred in the microenvironment of tumor cells^[3]. GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) (IC50s: 1.9 and 14 nM for LDHA and LDHB, respectively). GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR (EC50=10 μM). LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells. GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels range from 400 nM to no effect (EC50 reported as 30 μM). GSK2837808A (p.o.; 50 mg/kg in rats; 100 mg/kg in mice) treatment, causes blood compound levels at or below the detection limit of 2.5 ng/mL. Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is displayed to be 69 mL/minute/kg in rats and it exceeds the animal liver blood flow^[4].
参考文献

[1] Billiard J, Dennison JB, Briand J, Annan RS, Chai D, Colón M, Dodson CS, Gilbert SA, Greshock J, Jing J, Lu H, McSurdy-Freed JE, Orband-Miller LA, Mills GB, Quinn CJ, Schneck JL, Scott GF, Shaw AN, Waitt GM, Wooster RF, Duffy KJ. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19. doi: 10.1186/2049-3002-1-19. PMID: 24280423; PMCID: PMC4178217.
[2] Subramaniapillai Kolappan,et al. Structures of lactate dehydrogenase A (LDHA) in apo, ternary and inhibitor-bound forms. Acta Crystallogr D Biol Crystallogr. 2015 Feb;71(Pt 2):185-95.
[3] Farzaneh Jafary,et al. Novel Peptide Inhibitors for Lactate Dehydrogenase A (LDHA): A Survey to Inhibit LDHA Activity via Disruption of Protein-Protein Interaction. Sci Rep. 2019 Mar 18;9(1):4686.
[4] Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5394 mL
- 7.6968 mL
- 15.3936 mL
- 5 mM
- 0.3079 mL
- 1.5394 mL
- 3.0787 mL
- 10 mM
- 0.1539 mL
- 0.7697 mL
- 1.5394 mL

技术信息

CAS号	1445879-21-9	储存条件	粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C31H25F2N5O7S	运输	蓝冰
分子量	649.62	别名	GSK-2837808

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